Synthesis and evaluation of 3-aroylindoles as anticancer agents: Metabolite approach

Yu Shan Wu, Mohane Selvaraj Coumar, Jang Yang Chang, Hsu Yi Sun, Fu Ming Kuo, Ching Chuan Kuo, Ying Jun Chen, Chi Yen Chang, Chia Ling Hsiao, Jing Ping Liou, Ching Ping Chen, Hsien Tsung Yao, Yi Kun Chiang, Uan Kang Tan, Chiung Tong Chen, Chang Ying Chu, Su Ying Wu, Teng Kuang Yeh, Chin Yu Lin, Hsing Pang Hsieh

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BPR0L075 (2) is a potential anticancer drug candidate designed from Combretastatin A-4 (1) based on the bioisosterismprinciple.Metabolites of 2, proposed from in vitrohumanmicrosome studies,were synthesized, leading to the identification of metabolite-derived analogue 10 with 40-350 pM potency against various cancer cell lines. Insights gained from the major inactive metabolite of 2 led to the development of 29, with better pharmacokinetics and improved potency in the tumor xenograft model than 2.

Original languageEnglish
Pages (from-to)4941-4945
Number of pages5
JournalJournal of Medicinal Chemistry
Issue number15
Publication statusPublished - Aug 13 2009


ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

Cite this

Wu, Y. S., Coumar, M. S., Chang, J. Y., Sun, H. Y., Kuo, F. M., Kuo, C. C., Chen, Y. J., Chang, C. Y., Hsiao, C. L., Liou, J. P., Chen, C. P., Yao, H. T., Chiang, Y. K., Tan, U. K., Chen, C. T., Chu, C. Y., Wu, S. Y., Yeh, T. K., Lin, C. Y., & Hsieh, H. P. (2009). Synthesis and evaluation of 3-aroylindoles as anticancer agents: Metabolite approach. Journal of Medicinal Chemistry, 52(15), 4941-4945.